Esterase mutation is a mechanism of resistance to antimalarial compounds

Pepstatin is a known inhibitor of malarial proteases, but its activity varies between sources. Here, Istvanet al. identify a pepstatin ester as the active component of pepstatin preparations and show that this prodrug is activated by a Plasmodiumesterase, mutation of which can confer resistance to p...

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Autores principales: Eva S. Istvan, Jeremy P. Mallari, Victoria C. Corey, Neekesh V. Dharia, Garland R. Marshall, Elizabeth A. Winzeler, Daniel E. Goldberg
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2017
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Acceso en línea:https://doaj.org/article/1d38f9612f4048a39eb045aecf7bcf36
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Sumario:Pepstatin is a known inhibitor of malarial proteases, but its activity varies between sources. Here, Istvanet al. identify a pepstatin ester as the active component of pepstatin preparations and show that this prodrug is activated by a Plasmodiumesterase, mutation of which can confer resistance to pepstatin and other compounds.